AU2015213106B2 - Cytotoxic tubulysin compounds for conjugation - Google Patents

Cytotoxic tubulysin compounds for conjugation Download PDF

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Publication number
AU2015213106B2
AU2015213106B2 AU2015213106A AU2015213106A AU2015213106B2 AU 2015213106 B2 AU2015213106 B2 AU 2015213106B2 AU 2015213106 A AU2015213106 A AU 2015213106A AU 2015213106 A AU2015213106 A AU 2015213106A AU 2015213106 B2 AU2015213106 B2 AU 2015213106B2
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AU2015213106A1 (en
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Wolfgang Richter
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TUBE PHARMACEUTICALS GmbH
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TUBE PHARMACEUTICALS GmbH
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
AU2015213106A 2014-01-28 2015-01-28 Cytotoxic tubulysin compounds for conjugation Active AU2015213106B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14000291.6 2014-01-28
EP14000291 2014-01-28
PCT/EP2015/000161 WO2015113760A1 (en) 2014-01-28 2015-01-28 Cytotoxic tubulysin compounds for conjugation

Publications (2)

Publication Number Publication Date
AU2015213106A1 AU2015213106A1 (en) 2016-09-01
AU2015213106B2 true AU2015213106B2 (en) 2019-07-25

Family

ID=50028724

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2015213106A Active AU2015213106B2 (en) 2014-01-28 2015-01-28 Cytotoxic tubulysin compounds for conjugation

Country Status (8)

Country Link
US (2) US10183970B2 (ja)
EP (1) EP3099681B1 (ja)
JP (1) JP6664329B2 (ja)
CN (1) CN106132959B (ja)
AU (1) AU2015213106B2 (ja)
CA (1) CA2940311C (ja)
ES (1) ES2843537T3 (ja)
WO (1) WO2015113760A1 (ja)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2843537T3 (es) * 2014-01-28 2021-07-19 Tube Pharmaceuticals Gmbh Compuestos citotóxicos de tubulisina y conjugados de los mismos
GB201402006D0 (en) 2014-02-06 2014-03-26 Oncomatryx Biopharma S L Antibody-drug conjugates and immunotoxins
GB201402009D0 (en) 2014-02-06 2014-03-26 Oncomatryx Biopharma S L Antibody-drug conjugates and immunotoxins
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
EP3383420B1 (en) 2015-12-04 2022-03-23 Seagen Inc. Conjugates of quaternized tubulysin compounds
EP3411371A1 (en) * 2016-02-01 2018-12-12 Pfizer Inc Tubulysin analogs and methods for their preparation
JP2019515880A (ja) 2016-03-16 2019-06-13 エンドサイト・インコーポレイテッドＥｎｄｏｃｙｔｅ， Ｉｎｃ． 炭酸無水酵素ｉｘ阻害剤抱合体およびその使用
AU2017234676A1 (en) 2016-03-16 2018-09-20 Purdue Research Foundation Carbonic anhydrase IX targeting agents and methods
CN108779146B (zh) * 2016-03-29 2022-03-18 东丽株式会社 肽衍生物及其用途
JP2022516427A (ja) * 2018-12-21 2022-02-28 レゲネロン ファーマシューティカルス，インコーポレーテッド ツブリシン及びタンパク質－ツブリシンコンジュゲート
BR112022024361A2 (pt) * 2020-06-24 2022-12-27 Regeneron Pharma Tubulisinas e conjugados de proteína-tubulisina

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005112919A2 (en) * 2004-05-19 2005-12-01 Medarex, Inc. Self-immolative linkers and drug conjugates
US20110027274A1 (en) * 2009-08-03 2011-02-03 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
WO2012171020A1 (en) * 2011-06-10 2012-12-13 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
US20130116195A1 (en) * 2009-12-04 2013-05-09 Christopher Paul Leamon Binding ligand linked drug delivery conjugates of tubulysins
WO2013085925A1 (en) * 2011-12-05 2013-06-13 Igenica, Inc. Antibody-drug conjugates and related compounds, compositions, and methods
WO2013149185A1 (en) * 2012-03-29 2013-10-03 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
WO2013173391A1 (en) * 2012-05-15 2013-11-21 Concortis Biosystems, Corp Drug-conjugates, conjugation methods, and uses thereof
WO2014008375A1 (en) * 2012-07-05 2014-01-09 Mersana Therapeutics, Inc. Terminally modified polymers and conjugates thereof
WO2014040752A1 (en) * 2012-09-17 2014-03-20 Ontochem Gmbh Receptor ligand linked cytotoxic molecules
WO2014078484A1 (en) * 2012-11-15 2014-05-22 Endocyte, Inc. Conjugates for treating diseases caused by psma expressing cells
WO2014197871A2 (en) * 2013-06-06 2014-12-11 Igenica Biotherapeutics, Inc. Antibody-drug conjugates, compositions and methods of use

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Publication number Priority date Publication date Assignee Title
MXPA02012795A (es) * 2000-06-28 2004-07-30 Teva Pharma Carvedilol.
AU2003253048A1 (en) * 2002-07-09 2004-01-23 Morphochem Aktiengellschaft Fur Kombinatorische Chemie Tubulysin conjugates
DE10254439A1 (de) * 2002-11-21 2004-06-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
WO2008106080A2 (en) * 2007-02-27 2008-09-04 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Synthesis of desacetoxytubulysin h and analogs thereof
CA2807511A1 (en) * 2010-08-06 2012-02-09 Endocyte, Inc. Processes for preparing tubulysins
AU2012385228B2 (en) 2012-07-12 2016-10-06 Hangzhou Dac Biotech Co., Ltd Conjugates of cell binding molecules with cytotoxic agents
ES2843537T3 (es) * 2014-01-28 2021-07-19 Tube Pharmaceuticals Gmbh Compuestos citotóxicos de tubulisina y conjugados de los mismos

Patent Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005112919A2 (en) * 2004-05-19 2005-12-01 Medarex, Inc. Self-immolative linkers and drug conjugates
US20110027274A1 (en) * 2009-08-03 2011-02-03 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
US20130116195A1 (en) * 2009-12-04 2013-05-09 Christopher Paul Leamon Binding ligand linked drug delivery conjugates of tubulysins
WO2012171020A1 (en) * 2011-06-10 2012-12-13 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
WO2013085925A1 (en) * 2011-12-05 2013-06-13 Igenica, Inc. Antibody-drug conjugates and related compounds, compositions, and methods
WO2013149185A1 (en) * 2012-03-29 2013-10-03 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
WO2013173391A1 (en) * 2012-05-15 2013-11-21 Concortis Biosystems, Corp Drug-conjugates, conjugation methods, and uses thereof
WO2014008375A1 (en) * 2012-07-05 2014-01-09 Mersana Therapeutics, Inc. Terminally modified polymers and conjugates thereof
WO2014040752A1 (en) * 2012-09-17 2014-03-20 Ontochem Gmbh Receptor ligand linked cytotoxic molecules
WO2014078484A1 (en) * 2012-11-15 2014-05-22 Endocyte, Inc. Conjugates for treating diseases caused by psma expressing cells
WO2014197871A2 (en) * 2013-06-06 2014-12-11 Igenica Biotherapeutics, Inc. Antibody-drug conjugates, compositions and methods of use

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
P. SREEJITH SHANKAR ET AL, "Synthesis and cytotoxicity evaluation of diastereoisomers and N-terminal analogues of tubulysin-U", TETRAHEDRON LETTERS, (2013), vol. 54, no. 45, pages 6137 - 6141 *
RUI WANG ET AL, "Stereoselective Total Synthesis of Tubulysin V", CHINESE JOURNAL OF CHEMISTRY, (2013), vol. 31, no. 1, pages 40 - 48 *

Also Published As

Publication number Publication date
JP2017507926A (ja) 2017-03-23
CN106132959A (zh) 2016-11-16
AU2015213106A1 (en) 2016-09-01
US10183970B2 (en) 2019-01-22
EP3099681B1 (en) 2020-12-09
US20190233471A1 (en) 2019-08-01
ES2843537T3 (es) 2021-07-19
CA2940311A1 (en) 2015-08-06
CN106132959B (zh) 2020-04-17
WO2015113760A1 (en) 2015-08-06
CA2940311C (en) 2022-12-13
US10889616B2 (en) 2021-01-12
US20160340386A1 (en) 2016-11-24
EP3099681A1 (en) 2016-12-07
JP6664329B2 (ja) 2020-03-13

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